Modafinil, adrafinil and armodafinil

The modafinil is a stimulant of the central nervous system used for narcolepsy, other sleep disorders and ADHD. This substance is marketed in Italy as Provigil, in other countries such as Modalert, Alertex and Modapro. Armodrafinil (Nuvigil) is the Rfarmacologically most active isomer of modafinil. The adrafinilis a stimulant similar to modafinil used in France to treat the same ailments and is marketed as Olmifon. These substances, the modafinil in particular, are considered by some scholars of cognitive enhancers able also to improve memory and attention, some tests have been conducted and with 100 mg of modafinil there are positive results in memory and attention tests. Other research shows that at higher doses (300mg) the sense of fatigue decreases, motivation increases, reaction times, care and general cognitive functions accelerate (Baranski). These stimulants are also used to suppress sleep during night-time work. Modafinil is also a fatigue suppressor and is studied as an adjunct in various therapies with this intent, such as for depression. It also seems possible to use it as an appetite suppressant with amphetamine-like activity but with less side effects and risks of dependence.

The most common side effects are headache and nausea and all those typical effects of psychostimulants, although less marked than amphetamine (anxiety, agitation, insomnia, etc.). Modafinil has also been used in the last few decades by soldiers as a less dangerous amphetamine substitute.

Modafinil and adrafinil activate the noradrenergic, dopaminergic and serotoninergic systems, presumably by indirect action on transporters responsible for neurotransmitter reuptake. They are also α-1 adrenergic receptor agonists. The action appears to be distinctly different from traditional sympathomimetic stimulants such as amphetamine and ephedrine, in fact it does not produce hyperkinesis. It also appears that these substances increase the release of histamine in the brain, with unclear effects, also increase the excitatory gluttamatergic activity for the nervous system and reduce the depressing gabaergic activity of the nervous system.

The sum of these effects determines a strong stimulating action of the nervous system.

These substances can be found in urine for about 10 days. It is not known whether modafinil is able to improve athletic performance; however since it was included in the list of doping drugs in 2004 there have been some cases of positivity to it.

Imidazole derivatives are topically sympathomimetic vasoconstrictors with α-adrenergic activity used for nasal decongestants and for ophthalmic treatments (Rinazina, Vicks Sinex etc.). topical application of these substances acts on α-1-producing receptors producing constriction and reduces the production of exudate (mucus), freeing the airways.

According to RXShopMD.com, these substances are moderately active at central level and are currently not considered doping if used for topical use, however, a more marked use or even systemic intake has a certain stimulating effect.

However in the past they were present in the list of prohibited products and in fact it is possible that a use at high dosages, also referred to as nasal sprays (numerous sprays per nostril), may have ergogenic effects in terms of resistance.

Here is the full video about modafinil:

Octopamine (p-octopamine)

Octopamine was discovered in the octopus salivary glands. This substance is also an alkaloid of citrus aurantium. It seems that this substance acts as a transceiver replacing norepinephrine , in fact it is used as a replacement in long-term therapies with MAO inhibitors, moreover it has emerged that octopamine is an adrenoceptor agonist, in fact it acts as α- adrenergic in hypotensive states.

Octopamine also appears to be an β3-adrenergic receptor agonist capable of promoting lipolysis in adipocytes and fat loss, and once metabolized by monoamine oxidase it produces a substance with an insulin-like action.

The noradrenergic action allows the octopamine to improve muscle oxygenation, also improving the availability of energetic unbalanced substances as promoter of lipolysis and improvement of glucose absorption by the muscles. These actions guarantee the substance an ergogenic effect useful to athletes especially endurance. There have been several cases of positivity for octopamine in recent years.

Norfenilefrina (m- octopamine)

Norfenilefrina is an isomer of octopamine, it is an α-agonist for the treatment of hypotension. Studies on this substance are few, therefore its activity is not known in detail, but it remains a substance prohibited by the anti-doping regulation in quantity or nature similar to octopamine.